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Eptifibatide
Các tên gọi khác (2) :
  • Integrelin
  • Intrifiban
platelet aggregation inhibitors
Thuốc Gốc
Biotech
CAS: 188627-80-7
ATC: B01AC16
ĐG : Assia Chemical Industries Ltd.
CTHH: C35H49N11O9S2
PTK: 831.9620
Synthetic cyclic hexapeptide that binds to platelet receptor glycoprotein and inhibits platelet aggregation.
Nhận Dạng Quốc Tế & Đặc Tính Hóa Học
Công thức hóa học
C35H49N11O9S2
Phân tử khối
831.9620
Độ kỵ nước
-2.3
Dược Lực Học : Eptifibatide is an anti-coagulant that selectively blocks the platelet glycoprotein IIb/IIIa receptor. Eptifibatide is a cyclic heptapeptide derived from a protein found in the venom of the southeastern pygmy rattlesnake (Sistrurus miliarus barbouri). It belongs to the class of the so called arginin-glycin-aspartat-mimetics and reversibly binds to platelets.
Cơ Chế Tác Dụng : Synthetic cyclic hexapeptide that binds to platelet receptor glycoprotein and inhibits platelet aggregation. Eptifibatide inhibits platelet aggregation by reversibly binding to the platelet receptor glycoprotein (GP) IIb/IIIa of human platelets, thus preventing the binding of fibrinogen, von Willebrand factor, and other adhesive ligands. Inhibition of platelet aggregation occurs in a dose- and concentration-dependent manner.
Dược Động Học :

▧ Protein binding :
Approximately 25%
▧ Metabolism :
No major metabolites have been detected in human plasma. Deamidated eptifibatide and other, more polar metabolites have been detected in urine.
▧ Half Life :
Approximately 2.5 hours
▧ Clearance :
* 55 mL/kg/h [patients with coronary artery disease]
Độc Tính : Eptifibatide was not lethal to rats, rabbits, or monkeys when administered by continuous intravenous infusion for 90 minutes at a total dose of 45 mg/kg (about 2 to 5 times the recommended maximum daily human dose on a body surface area basis)
Chỉ Định : For treatment of myocardial infarction and acute coronary syndrome.
Tương Tác Thuốc :
  • Apixaban Monitor therapy due to potential risk of bleeding.
  • Collagenase Monitor therapy due to increased adverse effects of collagenase including risk of injection site bruising or bleeding.
  • Dabigatran etexilate Monitor therapy due to increased bleeding.
  • Dasatinib Monitor therapy due to enhanced anticoagulant effect.
  • Ginkgo biloba Additive anticoagulant/antiplatelet effects may increase bleed risk. Concomitant therapy should be avoided.
  • Glucosamine Monitor therapy due to enhanced antiplatelet effect.
  • Ibritumomab Monitor therapy due to enhanced adverse effects, ie bleeding of ibritumomab.
  • Obinutuzumab Monitor therapy due to increased risk of bleeding events.
  • Pentosan Polysulfate Pentosan can potentiate adverse effects of antiplatelet agents and thus increase bleeding risk. Combination must be used with caution.
  • Pentoxifylline Monitor therapy due to enhanced antiplatelet effect.
  • Rivaroxaban Consider modifying therapy due to enhanced anticoagulant effect.
  • Tipranavir Monitor therapy due to increased antiplatelet effect.
  • Tirofiban Additive effects. Concomitant use is contraindicated.
  • Treprostinil The prostacyclin analogue, Treprostinil, increases the risk of bleeding when combined with the antiplatelet agent, Eptifibatide. Monitor for increased bleeding during concomitant thearpy.
Liều Lượng & Cách Dùng : Solution - Intravenous
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